13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 5mg |
| CAS | 1332075-63-4 |
| 別名 | N/A |
| 化學名 | N/A |
| 分子式 | C28H33FN6O2 |
| 分子量 | 504.6 |
| 溶解度 | Soluble in DMSO |
| 儲存條件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述：
PI3kδ inhibitor 1 is a potent and selective PI3Kδ inhibitor with an IC50 of 3.8 nM. PI3Kδ|3.8 nM (IC50)
PI3kδ inhibitor 1 (Compound 3) is a potent inhibitor of PI3Kδ that is 200-400 fold selective for all three remaining Class I PI3K isoforms and extremely selective relative to 239 kinases tested in SelectScreen service (0/239 kinases showing >50% inhibition when tested at 1 μM; mTOR, DNA-PK, VPS34, PI4Kα and PI4Kβ are inhibited at 10% or less when tested at 1 μM; PIKC2A and PIKC2B are inhibited at 11% and 42%, respectively, at this same concentration and show less than 10% inhibition when tested at 0.1 μM; the PIKK family kinases ATM and ATR are not assessed)[1].
The pharmacokinetic properties of PI3kδ inhibitor 1 (Compound 3) are evaluated in mice and rats when dosed IV and orally. Good plasma exposures and reasonable half-lives are observed upon oral dosing, a reflection of high oral bioavailability (80% and 90% at a low dose for mouse and rat, respectively), moderate volume of distribution, and moderate clearance. PI3kδ inhibitor 1 has moderate terminal elimination half-life (t1/2=2.6 h, 2.9 h, 5 h, 2.6, 3.8 and 4.8 h for mouse (5 mg/kg, po), mouse (20 mg/kg, po), mouse (40 mg/kg, po), rat (5 mg/kg, po), rat (10 mg/kg, po), rat (30 mg/kg, po)). Plasma exposures and Cmax levels increase with dose in both mice and rats, important in that inflammatory disease models utilize these two species. Plasma protein binding for PI3kδ inhibitor 1 ranges from 80-88% in rodents and is consistent with values obtained in human plasma (86%)[1].
[1]. Sutherlin DP, et al. Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4296-302.
特別提醒：
1. 本產品僅供科研使用。請勿用于醫藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區。
2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。
原創作者：上海莼試生物技術有限公司
留言注意事項：
1.遵守中華人民共和國有關法律、法規，尊重網上道德，承擔一切因您的行為而直接或間接引起的法律責任。
2.請您真實的反映產品的情況,不要捏造、誣蔑、造謠。如對產品有任何疑問,也可以留言咨詢。
3.未經本站同意，任何人不得利用本留言簿發布個人或團體的具有廣告性質的信息或類似言論。
| 您感興趣的產品* | |
| 您的單位* | |
| 聯系人* | |
| 聯系電話* | |
| 詳細地址* | |
| 常用郵箱* | |
| 請輸入您對我們的意見或建議* | |
| 驗證碼* | |
 |
產品訂購說明:
1、報價含普票、運費。
2、常用試劑備貨充足，除對溫度要求極其嚴格的產品當天可發貨。
3、進口原裝產品要3-6周的貨期，詳細情況請咨詢客服。
4、訂貨時間為工作日每周一至周五16:00之前。
5、如需代為檢測，標本對環境溫度高，可聯系客服安排專人取樣（限省內客戶）。
6、代測免收代測費，一周出結果。
7、產品因運輸途中包裝破損請拒絕簽收，做退回。我們將在24小時之內為您補發 損壞產品。
8、如因單位財務制度原因，可申請先發貨，報賬后付款（此條款僅限醫院、學校信譽良好客戶）。
普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
關于莼試
產品訂購
新手指南
幫助中心